FR2817748A1 - Use of extracts of the crustacean Artemia salina in cosmetic and dermatological compositions to facilitate ion passage into cells and so effect skin hydration - Google Patents

Abstract

Use of Artemia salina extract in cosmetic and dermatological compositions to activate or facilitate the penetration of ions into cells.

Description

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The invention relates to the use in a cosmetic and / or dermatological composition, or for the preparation of such a composition, of an effective amount of an extract of artemis salina, the extract or the composition being intended to activate and / or facilitate the penetration of ions into the cell.

The ions represent a significant percentage of the dry mass of man. For example, calcium can be estimated at 1050 grams for a body of 70 kg, and for the same body, potassium represents 245 grams and sodium 105 grams. These ions are involved in many mechanisms, including cell homeostasis.

Sodium and potassium regulate the body's water content, and help maintain the acid-base balance. They are necessary for the excitability of nerve and muscle fibers. It is also necessary for protein synthesis and the storage of glycogen.

Calcium is involved, among other things, in the differentiation of keratinocytes.

At the cellular level, the intracellular potassium concentration is 140 mM, while the extracellular concentration is 5 mM. For sodium it is 5 to 15 mM against 145 mM extracellular, while for calcium, it is less than 0. 0001 mM against 1 to 2 mM extracellular.

The proper regulation of the fluxes of these ions through the cell membrane is necessary for life in general and for the skin in particular.

This regulation is carried out by active and passive transport across the cell membrane, in particular by means of ion channels.

The cosmetic and dermatological industry is very attentive to the hydro-mineral balance of the skin. Many preparations contain high ionic concentrations provided by minerals or plant or animal extracts.

These preparations tend to establish an osmotic gradient to facilitate the penetration of ions into cells.

Several studies have shown the harmful influence of certain ions, in topical application, on the skin barrier, one of the consequences of which is the increase in the insensible loss in

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eau, signe de la déshydratation de la peau. Or, l'hydratation est un élément essentiel de la cosmétique et de la dermatologie. On constate donc que subsiste le besoin d'une composition apportant des ions dans les cellules cutanées, mais sans les inconvénients de l'art antérieur.

water, a sign of dehydration of the skin. However, hydration is an essential element of cosmetics and dermatology. It can therefore be seen that there remains the need for a composition providing ions in the skin cells, but without the drawbacks of the prior art.

The Applicant has surprisingly found that the application of an effective amount of an extract of Artemia salina makes it possible to activate and / or facilitate the penetration of ions into the cell, without increasing the insensitive loss of water. , so without dehydrating the skin.

Artemia sa / M extracts are already used in cosmetics, but no one has, to date, established a link between an Artemia salina extract and intracellular ion penetration.

Also, the present invention relates to the use in a cosmetic and / or dermatological composition, or for the preparation of such a composition, of an effective amount of an extract of Artemia salina, the extract or the composition being intended to activate and / or facilitate the penetration of ions into the cell.

Thereafter, the term extract of Artemia Mina must be understood by extract of Artemia salina in a dormant state.

Indeed, Artemia salina is a small crustacean that lives in brackish waters. When environmental conditions become difficult (dehydration, increase in the mineral content), Artemia is encapsulated and enters a dormant phase, in which it can remain for several years. We often speak of Artemia egg. When conditions become favorable again, Artemia rehydrates and resumes its development cycle harmoniously.

One of the main biotopes for artemis salina is the Great Salt Lake, a salt lake in Utah, USA. This salt lake undergoes a natural process of evaporation of water, which produces a very high concentration of minerals in the lake. It is estimated that Great Salt Lake contains five million tonnes of minerals, a concentration of about eight

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fois supérieure à celle observée dans l'océan. Ces fluctuations font que seuls quelques organismes comme Artemia salina sont adaptés à cet environnement hyperminéralisé.

times greater than that observed in the ocean. These fluctuations mean that only a few organisms like Artemia salina are adapted to this hyper-mineralized environment.

Due to its environment, Artemia salina has developed important adaptive skills:
It has acquired a molecular display: the synthesis of GP4G (diguanosine tetraphostate), energy molecule precursor of ATP, GTP and activator of G proteins. (1)
It has cells specialized in regulating osmolarity, a corollary of the good hydro-mineral balance of plankton. (2) (1) AP4A and other dinucleotides tetraphosphates-McLennan CRC press (2) De novo purine synthesis in the crustacean Artemia: Influence of the salinity and geographical origin-J Comp Physiology B (1992) 162 263-266 L'Artemia salina will be used in its dormant state, to produce an extract intended to activate and / or facilitate the penetration of ions into the cell.

By penetration of ions into the cell is meant any active or passive transport of ions through the cell membrane. For example, we can cite potassium channels.

The potassium channels are present in all living cells, they act on a large number of functions including the regulation of cell volume, ion flow and cell differentiation.

This diversity of action comes, among other things, from the multiplicity of channel forms.

In mammals, there are 3 families of potassium channels:
The shaker family (6TMS / 1P) is the most extensive with more than 25 genes coding for proteins with 6 transmembrane domains and a short region (P domain) involved in the formation of the selective K + pore.

 The IRK mward family correct K + for at least 14 genes coding for proteins with 2 transmembrane domains and one P domain (2TMS / 1P).

 The third family (4TMS / 2P), discovered more recently, groups together several genes coding for proteins with 4 transmembrane domains and two P domains.

Channel activation: (Arrighi et al., 1998)

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Les canaux shaker sont soit voltage-dépendants, soit activés par les ions Ca2+.

The shaker channels are either voltage-dependent or activated by Ca2 + ions.

The IRK family channels are either coupled to G proteins or dependent on ATP (Challinor-Rogers and McPherson, 1994).

 The channels of the 4TMS / 2P family, although still little studied, are known to be activated by K + ions.

Several studies highlight the presence of potassium channels in human skin. At the cellular level, studies have been carried out on keratinocytes (Harmon et al., 1993; Mauro et al., 1997), fibroblasts (Estacion, 1991) and epithelial cells of sweat glands (Huang et al., 1999) .

A study on the skin barrier shows the importance of potassium channels in homeostasis linked to the permeability of the epidermal barrier (Lee et al., 1994).

The Artemia extract will allow the activation of the three types of potassium channels: - some shaker channels will be activated by Ca ions, - the IRK family channels will be activated because they are coupled to proteins
G, or ATP dependent, - the channels of the 4TMS / 2P family will be activated by K + ions.

Indeed, by its biotope, Artemia is naturally rich in ions, among others Ca and K +, which will be able to activate the ion channels. In addition, the properties of GP4G on the G and FATP proteins will further facilitate the transport of ions across the cell membrane.

Besides the transport of K + ions, the Artemia extract will facilitate the transport of Ca ++ ions. Indeed, the Applicant has been able to demonstrate that the Artemia extract induces the differentiation of keratinocytes (slowing down of cell growth, increased expression of keratin). However, this differentiation is a function of the Ca ions.

These in vitro studies were carried out on keratinocytes in culture by immunoblotting, showing the increase in keratins.

Other studies, ex vivo, have demonstrated the increase in keratin by hematoxylin and eosin staining, and have shown, by immunostaining, the increase in the expression of Pan-keratin and Filaggrin ( cell differentiation markers).

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Cependant, il ne faut pas oublier qu'une concentration trop importante en ions Ca et K+ à la surface de la peau va entraîner un déséquilibre de la barrière cutanée qui se traduit par une augmentation de la perte insensible en eau. L'extrait d'Artémia utilisé par la demanderesse, bien que riche en ions, n'affecte pas l'équilibre de la barrière cutanée, ainsi que montré dans l'exemple 2.

However, it should not be forgotten that too high a concentration of Ca and K + ions on the surface of the skin will lead to an imbalance of the skin barrier which results in an increase in the insensible loss of water. The Artemia extract used by the applicant, although rich in ions, does not affect the balance of the skin barrier, as shown in Example 2.

The subject of the invention is also the use in a cosmetic and / or dermatological composition, or for the preparation of such a composition, of an effective amount of an extract of Artemia salina, characterized in that the penetration of ions in the cell will hydrate the cell.

The ion transport mechanisms, seen above, will facilitate the passage of ions through the cell membrane, and in so doing they transport water molecules which will hydrate the cell. Indeed, by a phenomenon of solvation, the ions will fix a certain number of water molecules, according among other things, to their degree of electronegativity. So in a very short time, a slight phenomenon of hydration will accompany the transport of the ions towards the interior of the cell. This result is repeated in Example 3.

In a second step, the differentiation of the keratinocytes accompanying the intracellular transport of Cash ions, will strengthen the skin barrier and thus limit the dehydration of the epidermis.

To give an order of magnitude, in the cosmetic or dermatological compositions of the present invention, an extract as defined above can be used, in an amount representing from 0.01% to 20% of the total weight of the composition and preferably in an amount representing from 0.1% to 10% of the total weight of the composition.

Preferably, the compositions according to the present invention will be in a form suitable for administration by the topical skin route, and cover all cosmetic or dermatological forms. These compositions may in particular be in the form of creams, O / W emulsions, W / O or multiple emulsions, solutions,

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 suspensions, gels, milks, lotions, sticks or even powders, suitable for application to the skin, lips and / or hair.

These compositions include the excipients necessary for their formulation, such as solvents, thickeners, diluents, surfactants, antioxidants, dyes, preservatives, perfumes.

Of course, those skilled in the art will take care to choose any additional compounds, active or non-active, and / or their quantity, so that the advantageous properties of the extract of ArtemMa salina are not, or not substantially , altered by the planned addition.

Other advantages and characteristics of the invention will appear better on reading the examples given by way of illustration and without limitation.

EXAMPLE 1-PREPARATION OF AN EXTRACT OF ARTEMIA SALINA 50 grams of Artemia eggs, therefore of Artemia salina in a dormant state, are rehydrated from 30 minutes to 6 hours in 1 liter of distilled water, at a temperature ranging from 30 oC to 75 cl, in a suitable medium, mainly consisting of water, and at a pH between 4 and 7. Then, these eggs are ground. The extract thus obtained is centrifuged and filtered.

The extract is then treated and sterilized to comply with cosmetic requirements (color, odor, appearance, sterility ...).

EXAMPLE 2-EFFECT OF THE EXTRACT OF EXAMPLE 1 ON THE LOSS
WATER INSENSITIVE (TEWL) The study allows to evaluate the effectiveness of the product on the insensitive water loss of the skin.

The study was conducted on 12 volunteers including 7 men and 5 women, aged 21 to 52 years.

According to the volunteers, the nature of the skins was normal or dry, with no skin pathology, and the melanic index from 2 to 4.

The test was carried out in single blind, and its duration was 2 hours.

Areas of 30 cm2 have been defined on the right and left forearms, at the wrists. The extract of Artemia salina from Example 1 was applied to one side, and the

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placebo sur l'autre.

placebo on the other.

The amount of product applied was 2, 3 mg per cm2 or 70 (it for 30 cm2 The insensitive water loss (TEWL Trans Epidermal Water Loss) was evaluated using the Dermalabo evaporimeter (Cortex Technology). The measurement is expressed in g / m / h and is interrupted when the standard deviation is 0.1 or after 60 seconds. The measurement was carried out under controlled conditions of temperature and humidity (22 C 1 and 50 % 5).

Procedure: 1) Basal measurements, 2) Application of products, 3) Measurements at T15mn, T30mn and T2h.

Result: No modification of the TEWL between the two arms on the 12 volunteers.

Conclusion: The Artemia salina extract does not modify the insensitive water loss of the skin, therefore it does not unbalance the skin barrier.

EXAMPLE 3-EFFECT OF THE EXTRACT OF EXAMPLE 1 ON HYDRATION
SKIN The study allows to evaluate the effectiveness of the product on the hydration of the skin.

The study was conducted on 12 volunteers including 7 men and 5 women, aged 21 to 52 years.

According to the volunteers, the nature of the skins was normal or dry, with no skin pathology, and the melanic index from 2 to 4.

The test was carried out in single blind, and its duration was 2 hours.

Areas of 30 cm2 have been defined on the right and left forearms, at the wrists. The extract from M. salina from example 1 was applied on one side, and placebo on the other.

The amount of product applied was 2.3 mg per cm2 or 70 cl per 30 cm2.

The hydration of the skin was quantified using the CM825 corneometer (Courage and Khazaka Electronic, Köln, Germany). Capacitance (international unit), is a measure

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de la teneur en eau du stratum corneum. La valeur obtenue est la moyenne de 3 mesures répétées successivement sur la même zone.

the water content of the stratum corneum. The value obtained is the average of 3 measurements repeated successively on the same area.

Procedure: 1) Basal measurements, 2) Application of products, 3) Measurements at T15mn, T30mn and T2h.

Result: After 15 minutes, there is an average increase in hydration of 8.3%, which increases to 10.6% after 30 minutes to decrease to 8.0% after 2 hours. These values are understood by subtracting the hydration due to water from that due to Artemia extract.

Conclusion: Artemis salina extract has a slight hydrating effect on the skin, in line with the increased transport of ions across the cell membrane.

EXAMPLE 4-EXAMPLE OF COMPOSITIONS These compositions were obtained by simple mixing of the various components. The quantities indicated are given as a percentage by weight.

Parfum 0. 50 % Eau qsp 100 % 1-Oil in water emulsion Oily phase: * Montanov 68 (Cetearyl Alcohol and Cetearyl Glucoside) 5.00% # Jojoba oil 5. 00% # Vaseline oil 5. 00% "Isopropyl Palmitate 7.00% Aqueous phase: Glycerin 5. 00% Allantoin 0. 10% Extract from Example 1 5.00% Sepigel 305 (Polyacrylamide and C13-14 Isoparaffin and Laureth-7) 0.30% Preservative 0. 50%

Perfume 0. 50% Water qs 100%

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2-Gel Carbopol Ultrez 10 (sol. à 2%) 25. 00 % Triéthanolamine 0. 50 % Extrait de l'exemple 1 5. 00 % Conservateur 0. 20 % EDTA (sequestrant) 0. 10 % Parfum 0. 50 % Eau qsp 100 % 3-Lotion * Mono Propylene Glycol 1. 00 % . Allantoïne 0. 30 % . Glycerine 1. 00 % Cetiol HE (PEG-7 Glyceryl Cocoate) 1. 00 % "Extrait de l'exemple 1 5. 00 % "Conservateur 0. 20 % . Parfum 0. 50 % M Eau qsp 100 %

2-Carbopol Ultrez 10 Gel (2% sol.) 25. 00% Triethanolamine 0. 50% Extract from Example 1 5. 00% Preservative 0. 20% EDTA (sequestrant) 0. 10% Perfume 0. 50% Water qs 100% 3-Lotion * Mono Propylene Glycol 1. 00%. Allantoin 0.30%. Glycerin 1. 00% Cetiol HE (PEG-7 Glyceryl Cocoate) 1. 00% "Extract from Example 1 5. 00%" Preservative 0. 20%. Perfume 0. 50% M Water qs 100%

Claims (5)

 1. Use in a cosmetic and / or dermatological composition, or for the preparation of such a composition, of an effective amount of an extract of Artemia salina, the extract or the composition being intended to activate and / or facilitate the penetration of ions into the cell. 2. Use according to claim 1, characterized in that the penetration of ions into the cell will hydrate the cell. 3. Use according to any one of the preceding claims, characterized in that the extract of Artemia salina is used in an amount representing from 0.01% to 20% of the total weight of the composition. 4. Use according to claim 3, characterized in that the extract of Artemia satina is used in an amount representing from 0.1% to 10% of the total weight of the composition. 5. Use according to any one of the preceding claims, characterized in that the Artemia salina will be used in its dormant state.